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OSU-T315 (1,5-regioisomer) is a novel, potent and specific small molecule inhibitor of Integrin-linked kinase (ILK) with an IC50 of 0.6 μM, suppressing cancer cell proliferation in vitro and in vivo and inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.
Physicochemical Properties
| Molecular Formula | C30H30F3N5O |
| Molecular Weight | 533.6 |
| Exact Mass | 533.24 |
| CAS # | 1333146-24-9 |
| Related CAS # | 1333146-24-9; |
| PubChem CID | 51051074 |
| Appearance | White to light yellow solid powder |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 739.2±60.0 °C at 760 mmHg |
| Flash Point | 400.9±32.9 °C |
| Vapour Pressure | 0.0±2.4 mmHg at 25°C |
| Index of Refraction | 1.615 |
| LogP | 4.65 |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 7 |
| Heavy Atom Count | 39 |
| Complexity | 767 |
| Defined Atom Stereocenter Count | 0 |
| InChi Key | GHBUPSVATJKTRR-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C30H30F3N5O/c1-34-29(39)15-10-25-20-28(38(36-25)27-13-11-26(12-14-27)37-18-16-35-17-19-37)23-4-2-21(3-5-23)22-6-8-24(9-7-22)30(31,32)33/h2-9,11-14,20,35H,10,15-19H2,1H3,(H,34,39) |
| Chemical Name | N-Methyl-3-[1-(4-piperazin-1-yl-phenyl)-5-(4'-trifluoromethyl-biphenyl-4-yl)-1H-pyrazol-3-yl]-propionamide |
| Synonyms | ILK inhibitor 22(1,5) T315(1,5) OSU-T315 (1,5-regioisomer) OSUT315 OSU T315 OSU-T315 |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| References |
[1].Su-Lin Lee,et al Identification and Characterization of a Novel Integrin-Linked Kinase Inhibitor.J Med Chem. 2011 Sep 22; 54(18): 6364\u20136374 [2].Liu TM, et al. OSU-T315: a novel targeted therapeutic that antagonizes AKT membrane localization and activation of chronic lymphocytic leukemia cells. Blood. 2015 Jan 8;125(2):284-95. [3].OSU-T315 as an Interesting Lead Molecule for Novel B Cell-Specific Therapeutics. J Immunol Res. 2018 Sep 12;2018:2505818. doi: 10.1155/2018/2505818. eCollection 2018. PubMed PMID: 30276218; PubMed Central PMCID: PMC6157143. |
Solubility Data
| Solubility (In Vitro) | DMSO : ~50 mg/mL (~93.70 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (9.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (9.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8741 mL | 9.3703 mL | 18.7406 mL | |
| 5 mM | 0.3748 mL | 1.8741 mL | 3.7481 mL | |
| 10 mM | 0.1874 mL | 0.9370 mL | 1.8741 mL |